Expression of the type 2 receptor for cysteinyl leukotrienes (CysLT2R) by human mast cells: Functional distinction from CysLT1R

Proc Natl Acad Sci U S A. 2003 Sep 30;100(20):11589-93. doi: 10.1073/pnas.2034927100. Epub 2003 Sep 17.

Abstract

Cysteinyl leukotrienes (cysLTs) mediate vascular leakage and bronchoconstriction through the smooth muscle-associated CysLT type 1 receptor (CysLT1R), one of at least two loosely homologous cysLT-binding G protein-coupled receptors. We previously reported that CysLT1R is expressed by cultured human mast cells (hMCs), and that priming these cells with IL-4 enhances their sensitivity to calcium flux and cytokine generation in response to cys-LTs and the nucleotide ligand, uridine diphosphate (UDP), without increasing their surface expression of CysLT1R. We now report that hMCs express the type 2 receptor for cysLTs (CysLT2R) as well, and that the amount of surface CysLT2R protein increases in response to priming with IL-4. The selective function of CysLT2R was evident based on uninhibited IL-8 secretion by IL-4-primed hMCs stimulated with cys-LTs or UDP in the presence of the selective CysLT1R antagonist MK571. MK571 did inhibit IL-5 generation, calcium flux, and phosphorylation of extracellular signal-regulated kinase. IL-8 secretion was inhibited by pertussis toxin and a selective p38 kinase inhibitor, SB203580. The CysLT2 response may permit the cys-LTs and nucleotides generated in infection and tissue injury to elicit IL-8 generation by hMCs, potentially leading to neutrophilic infiltration, a characteristic of aerosol challenge-induced late-phase responses and of sudden death associated with asthma.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Enzyme Inhibitors / pharmacology
  • Humans
  • Imidazoles / pharmacology
  • Leukotriene Antagonists
  • Mast Cells / metabolism*
  • Membrane Proteins*
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors
  • Mitogen-Activated Protein Kinases / metabolism
  • Phosphorylation
  • Propionates / pharmacology
  • Pyridines / pharmacology
  • Quinolines / pharmacology
  • RNA, Messenger / genetics
  • Receptors, Leukotriene / genetics
  • Receptors, Leukotriene / metabolism*
  • Receptors, Leukotriene / physiology*

Substances

  • Enzyme Inhibitors
  • Imidazoles
  • Leukotriene Antagonists
  • Membrane Proteins
  • Propionates
  • Pyridines
  • Quinolines
  • RNA, Messenger
  • Receptors, Leukotriene
  • verlukast
  • cysteinyl leukotriene receptor 2
  • Mitogen-Activated Protein Kinases
  • leukotriene D4 receptor
  • SB 203580